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钙拮抗剂比较:药理学家的观点。

Calcium antagonists in comparison: view of the pharmacologist.

作者信息

Borchard U

机构信息

Institut für Pharmakologie, Heinrich-Heine-Universität Düsseldorf, Germany.

出版信息

J Cardiovasc Pharmacol. 1994;24 Suppl 2:S85-91.

PMID:7898100
Abstract

A great number of calcium antagonists are available for the treatment of cardiovascular diseases. Differences in pharmacodynamic and/or pharmacokinetic properties can be used to optimize therapy in patients and to minimize side effects. In contrast to all dihydropyridine (DHP) derivatives, drugs of the verapamil type slow atrioventricular conduction and are widely used for treatment of supraventricular tachycardia. The higher vasoselectivity of new DHP derivatives as compared with nifedipine should be regarded as an advantage for the treatment of patients with impaired left ventricular function. Besides vasodilation, additional effects such as antiatherosclerotic action, amelioration of rheological parameters, bronchial relaxation, or improvement of cerebral capacity in patients with cerebro-organic disorders have been documented for individual drugs. The long plasma half-life of some new calcium antagonists is advantageous with respect to patient compliance. Furthermore, a delayed increase in plasma concentration (high tmax values) is useful to minimize side effects such as reflex tachycardia, flush, headache, and dizziness.

摘要

有大量的钙拮抗剂可用于治疗心血管疾病。药效学和/或药代动力学特性的差异可用于优化患者的治疗并将副作用降至最低。与所有二氢吡啶(DHP)衍生物不同,维拉帕米类药物会减慢房室传导,广泛用于治疗室上性心动过速。与硝苯地平相比,新型DHP衍生物具有更高的血管选择性,这应被视为治疗左心室功能受损患者的一个优势。除血管舒张作用外,个别药物还具有抗动脉粥样硬化作用、改善流变学参数、支气管舒张或改善脑器质性疾病患者的脑功能等附加作用。一些新型钙拮抗剂的血浆半衰期较长,这对患者的依从性有利。此外,血浆浓度延迟升高(高tmax值)有助于将反射性心动过速、潮红、头痛和头晕等副作用降至最低。

相似文献

1
Calcium antagonists in comparison: view of the pharmacologist.钙拮抗剂比较:药理学家的观点。
J Cardiovasc Pharmacol. 1994;24 Suppl 2:S85-91.
2
Nilvadipine: profile of a new calcium antagonist. An overview.尼伐地平:一种新型钙拮抗剂的概况。综述。
J Cardiovasc Pharmacol. 1994;24 Suppl 2:S92-107.
3
Lercanidipine: short plasma half-life, long duration of action and high cholesterol tolerance. Updated molecular model to rationalize its pharmacokinetic properties.乐卡地平:血浆半衰期短、作用持续时间长且胆固醇耐受性高。更新分子模型以阐明其药代动力学特性。
Blood Press Suppl. 1998;2:10-7.
4
[Principles of the pharmacokinetics and pharmacodynamics of calcium antagonists].[钙拮抗剂的药代动力学和药效学原理]
Wien Med Wochenschr. 1993;143(19-20):490-500.
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Calcium channel antagonists. What do the second-generation agents have to offer?钙通道拮抗剂。第二代药物有哪些优势?
Postgrad Med. 1994 Jan;95(1):181-90.
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[Calcium channel blockers (calcium antagonists). Background, effects and use].[钙通道阻滞剂(钙拮抗剂)。背景、作用及用途]
Ugeskr Laeger. 1995 Jun 26;157(26):3750-4.
7
Pharmacological in vitro studies of the new 1,4-dihydropyridine calcium antagonist lercanidipine.新型1,4 - 二氢吡啶类钙拮抗剂乐卡地平的体外药理学研究
Arzneimittelforschung. 1996 Jan;46(1):15-24.
8
The pharmacological properties of lipophilic calcium antagonists.亲脂性钙拮抗剂的药理特性。
Blood Press Suppl. 1998;2:5-9.
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[Pharmacokinetics and pharmacodynamics of calcium channel blockers].[钙通道阻滞剂的药代动力学和药效学]
Vnitr Lek. 1995 Mar;41(3):164-6.
10
Critical assessment of calcium antagonists.钙拮抗剂的批判性评估
Aust Fam Physician. 1997 Jul;26(7):841-5, 847-8.

引用本文的文献

1
The nifedipine gastrointestinal therapeutic system (GITS). Evaluation of pharmaceutical, pharmacokinetic and pharmacological properties.硝苯地平胃肠道治疗系统(GITS)。药物、药代动力学和药理学特性评估。
Clin Pharmacokinet. 1996 Jan;30(1):28-51. doi: 10.2165/00003088-199630010-00003.
2
Nisoldipine coat-core. A review of its pharmacology and therapeutic efficacy in hypertension.尼索地平包衣片芯。其药理学及高血压治疗疗效综述。
Drugs. 1996 Aug;52(2):232-53. doi: 10.2165/00003495-199652020-00009.
3
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
1,4-二氢吡啶和吡啶衍生物与腺苷受体的相互作用:对A3受体的选择性
J Med Chem. 1996 Jul 19;39(15):2980-9. doi: 10.1021/jm9600205.
4
Nilvadipine. A review of its pharmacodynamic and pharmacokinetic properties, therapeutic use in hypertension and potential in cerebrovascular disease and angina.尼伐地平。对其药效学和药代动力学特性、在高血压治疗中的应用以及在脑血管疾病和心绞痛方面的潜力的综述。
Drugs Aging. 1995 Feb;6(2):150-71. doi: 10.2165/00002512-199506020-00007.